CA2864040A1 - Morpholinoalkyl fumarate compounds, pharmaceutical compositions, and methods of use - Google Patents

Morpholinoalkyl fumarate compounds, pharmaceutical compositions, and methods of use Download PDF

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Publication number
CA2864040A1
CA2864040A1 CA2864040A CA2864040A CA2864040A1 CA 2864040 A1 CA2864040 A1 CA 2864040A1 CA 2864040 A CA2864040 A CA 2864040A CA 2864040 A CA2864040 A CA 2864040A CA 2864040 A1 CA2864040 A1 CA 2864040A1
Authority
CA
Canada
Prior art keywords
pharmaceutical compositions
methods
morpholinoalkyl
disease
fumarate compounds
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2864040A
Other languages
French (fr)
Inventor
Kenneth C. Cundy
Suresh K MANTHATI
David J. Wustrow
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
XenoPort Inc
Original Assignee
XenoPort Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by XenoPort Inc filed Critical XenoPort Inc
Publication of CA2864040A1 publication Critical patent/CA2864040A1/en
Abandoned legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Morpholinoalkyl fumarates, pharmaceutical compositions comprising the morpholinoalkyl fumarates, and methods of using morpholinoalkyl fumarates and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.
CA2864040A 2012-02-07 2013-02-07 Morpholinoalkyl fumarate compounds, pharmaceutical compositions, and methods of use Abandoned CA2864040A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261595835P 2012-02-07 2012-02-07
US61/595,835 2012-02-07
PCT/US2013/025118 WO2013119791A1 (en) 2012-02-07 2013-02-07 Morpholinoalkyl fumarate compounds, pharmaceutical compositions, and methods of use

Publications (1)

Publication Number Publication Date
CA2864040A1 true CA2864040A1 (en) 2013-08-15

Family

ID=47720772

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2864040A Abandoned CA2864040A1 (en) 2012-02-07 2013-02-07 Morpholinoalkyl fumarate compounds, pharmaceutical compositions, and methods of use

Country Status (15)

Country Link
US (2) US8952006B2 (en)
EP (1) EP2812319A1 (en)
JP (1) JP5918395B2 (en)
KR (1) KR20140129136A (en)
CN (1) CN104169261A (en)
AU (1) AU2013203335B2 (en)
BR (1) BR112014019480A8 (en)
CA (1) CA2864040A1 (en)
IL (1) IL233941A0 (en)
MX (1) MX2014009511A (en)
NZ (1) NZ629728A (en)
RU (1) RU2014136394A (en)
TW (1) TWI486339B (en)
WO (1) WO2013119791A1 (en)
ZA (1) ZA201406145B (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10080733B2 (en) 2013-03-14 2018-09-25 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases
US11230548B2 (en) 2013-03-14 2022-01-25 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2477884T3 (en) 2008-08-19 2014-07-18 Xenoport, Inc. Methyl hydrogen hydrogen fumarate prodrugs, pharmaceutical compositions thereof and methods of use
WO2013181451A1 (en) * 2012-05-30 2013-12-05 Xenoport, Inc. Treatment of multiple sclerosis and psoriasis using prodrugs of methyl hydrogen fumarate
CA2882730C (en) * 2012-08-22 2019-12-31 Xenoport, Inc. Oral dosage forms of methyl hydrogen fumarate and prodrugs thereof
CA2882713A1 (en) * 2012-08-22 2014-02-27 Xenoport, Inc. Methods of administering monomethyl fumarate and prodrugs thereof having reduced side effects
WO2014031901A1 (en) * 2012-08-22 2014-02-27 Xenoport, Inc. Methods of use for monomethyl fumarate and prodrugs thereof
TW201436790A (en) * 2012-12-21 2014-10-01 Biogen Idec Inc Deuterium substituted fumarate derivatives
US10179118B2 (en) 2013-03-24 2019-01-15 Arbor Pharmaceuticals, Llc Pharmaceutical compositions of dimethyl fumarate
WO2014197860A1 (en) 2013-06-07 2014-12-11 Xenoport, Inc. Method of making monomethyl fumarate
WO2014205392A1 (en) 2013-06-21 2014-12-24 Xenoport, Inc. Cocrystals of dimethyl fumarate
TW201516020A (en) 2013-09-06 2015-05-01 Xenoport Inc Crystalline forms of (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, methods of synthesis and use
EP3049074A1 (en) * 2013-09-27 2016-08-03 ratiopharm GmbH Prodrugs of monomethyl fumarate (mmf)
WO2015082590A2 (en) * 2013-12-05 2015-06-11 Ratiopharm Gmbh Bis-mmf derivatives
ES2753361T3 (en) * 2014-02-24 2020-04-08 Alkermes Pharma Ireland Ltd Sulfonamide and sulfinamide fumarate prodrugs and their use in the treatment of various diseases
EP3119791B1 (en) 2014-03-21 2019-01-16 Université Paris-Est Créteil Val de Marne Fumarate-co-releasing molecule hybrids, their use in the treatment of inflammatory or cardiovascular diseases and their process of preparation
US9999672B2 (en) 2014-03-24 2018-06-19 Xenoport, Inc. Pharmaceutical compositions of fumaric acid esters
WO2016061393A1 (en) 2014-10-15 2016-04-21 Xenoport, Inc. Fumarate compounds, pharmaceutical compositions, and methods of use
US10170537B2 (en) 2014-12-23 2019-01-01 International Business Machines Corporation Capacitor structure compatible with nanowire CMOS
US9630934B2 (en) * 2015-02-08 2017-04-25 Mark Quang Nguyen Fumarate compounds, pharmaceutical compositions thereof, and methods of use
CN115957294A (en) 2015-05-28 2023-04-14 贝勒医学院 Beneficial effects of supplementation with N-acetylcysteine and glycine to improve glutathione levels
CN111065619B (en) * 2017-08-29 2022-08-12 浙江海正药业股份有限公司 (E) -alpha, beta-unsaturated amide compound, preparation method and application thereof
CN116307280B (en) * 2023-05-18 2023-08-01 成都理工大学 Quantitative evaluation method for sulfur blockage damage of reservoir of acid gas reservoir

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2163060A1 (en) * 1971-12-18 1973-06-20 Basf Ag Aqueous DISPERSIONS OF MIXED POLYMERIZES OF MONOESTERS OF UNSATURATED DICARBONIC ACIDS
DE19721099C2 (en) 1997-05-20 1999-12-02 Fumapharm Ag Muri Use of fumaric acid derivatives
DE19814358C2 (en) 1998-03-31 2002-01-17 Fumapharm Ag Muri Use of alkyl hydrogen fumarates for the treatment of psoriasis, psoriatic arthritis, neurodermatitis and enteritis regionalis Crohn
DE19839566C2 (en) 1998-08-31 2002-01-17 Fumapharm Ag Muri Use of fumaric acid derivatives in transplant medicine
DE19848260C2 (en) 1998-10-20 2002-01-17 Fumapharm Ag Muri Fumaric microtablets
DE19853487A1 (en) * 1998-11-19 2000-05-25 Fumapharm Ag Muri Use of dialkyl fumarate for treating transplant rejection and autoimmune disease
DE10000577A1 (en) 2000-01-10 2001-07-26 Fumapharm Ag Muri Treating mitochondrial diseases, e.g. Parkinson's or Alzheimer's disease or retinitis pigmentosa, using fumaric acid derivative, e.g. mono- or dialkyl fumarate, having succinate dehydrogenase stimulating activity
DE10101307A1 (en) 2001-01-12 2002-08-01 Fumapharm Ag Muri Fumaric acid derivatives as NF-kappaB inhibitor
RU2290946C2 (en) 2001-01-12 2007-01-10 Фумафарм Аг Fumaric acid amides
DE10217314A1 (en) 2002-04-18 2003-11-13 Fumapharm Ag Muri Carbocyclic and oxacarboncyclic fumaric acid oligomers
GB0320441D0 (en) * 2003-09-02 2003-10-01 Givaudan Sa Organic compounds
MXPA06002657A (en) 2003-09-09 2006-06-05 Fumapharm Ag The use of fumaric acid derivatives for treating cardiac insufficiency, and asthma.
DE10342423A1 (en) 2003-09-13 2005-04-14 Heidland, August, Prof. Dr.med. Dr.h.c. Use of fumaric acid derivatives for the prophylaxis and treatment of genome damage
EP2801354B1 (en) 2004-10-08 2017-02-08 Forward Pharma A/S Controlled release pharmaceutical compositions comprising a fumaric acid ester
US20080004344A1 (en) 2004-11-10 2008-01-03 Aditech Pharma Ab Novel Salts of Fumaric Acid Monoalkylesters and Their Pharmaceutical Use
DE102005022845A1 (en) 2005-05-18 2006-11-23 Fumapharm Ag Thiosuccinic acid derivatives and their use
WO2007042034A1 (en) 2005-10-07 2007-04-19 Aditech Pharma Ab Controlled release pharmaceutical compositions comprising a fumaric acid ester
CN101304732A (en) * 2005-10-07 2008-11-12 Adi技术制药股份公司 Controlled release pharmaceutical compositions comprising a fumaric acid ester
AU2007248473B2 (en) 2006-05-05 2011-01-27 The Regents Of The University Of Michigan Bivalent Smac mimetics and the uses thereof
ES2477884T3 (en) * 2008-08-19 2014-07-18 Xenoport, Inc. Methyl hydrogen hydrogen fumarate prodrugs, pharmaceutical compositions thereof and methods of use
WO2011085211A1 (en) * 2010-01-08 2011-07-14 Catabasis Pharmaceuticals, Inc. Fatty acid fumarate derivatives and their uses
EP2934507B1 (en) 2012-12-21 2017-05-31 ratiopharm GmbH Prodrugs of monomethyl fumarate (mmf)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10080733B2 (en) 2013-03-14 2018-09-25 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases
US10406133B2 (en) 2013-03-14 2019-09-10 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases
US10596140B2 (en) 2013-03-14 2020-03-24 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases
US11083703B2 (en) 2013-03-14 2021-08-10 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases
US11230548B2 (en) 2013-03-14 2022-01-25 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases
US11679092B2 (en) 2013-03-14 2023-06-20 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases
US11905298B2 (en) 2013-03-14 2024-02-20 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases

Also Published As

Publication number Publication date
JP5918395B2 (en) 2016-05-18
EP2812319A1 (en) 2014-12-17
US20130203753A1 (en) 2013-08-08
NZ629728A (en) 2016-07-29
US20140051705A1 (en) 2014-02-20
IL233941A0 (en) 2014-09-30
MX2014009511A (en) 2014-10-24
BR112014019480A2 (en) 2017-06-20
ZA201406145B (en) 2016-06-29
BR112014019480A8 (en) 2017-07-11
WO2013119791A1 (en) 2013-08-15
AU2013203335B2 (en) 2016-05-26
TW201343634A (en) 2013-11-01
AU2013203335A1 (en) 2013-08-22
CN104169261A (en) 2014-11-26
KR20140129136A (en) 2014-11-06
TWI486339B (en) 2015-06-01
US8952006B2 (en) 2015-02-10
RU2014136394A (en) 2016-03-27
JP2015508073A (en) 2015-03-16

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Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20140806

FZDE Discontinued

Effective date: 20171128